Eurand Pharmaceuticals, Ltd.

Eurand International S.p.a.

Aptalis Pharma Limited

Massimo Bresciani

Luca Dobetti

Fabio Carli

Tiziana Canal

Leonardo Rabaglia

Lorenzo Magarotto

Paolo Gambini

The present invention refers to a process to prepare a highly activated composite of one or more water-insoluble drugs, said process comprising the steps of: (a) subjecting said water-insoluble drug and a cross-linked polymer to co-grinding; (b) exposing the ground product of step a. to contact with water or water vapors. The resulting composite contains large amounts of drug in the easily soluble amorphous form, reduced amounts of drug in the nanocrystalline form, and is substantially free from practically insoluble drug crystals.

Process of thermodynamical activation of water-insoluble drugs loaded into cross-linked polymers

A process is described for the activation (increase in solubility and bioavailability) of drugs. The process, carried out in a vibrational mill, is characterised by the use of given proportions between the physical mixture made up of drug and pharmaceutical carrier and the empty volume among the grinding means contained inside the mill. The process leads to obtaining powders for pharmaceutical use in which the drug has a high and constant degree of activation; this result is obtainable irrespective of the nature of the drug and carrier used, and of their weight ratio.

Process for activation of drugs in a vibrational mill

The invention comprises a process for activating drugs by means of high-energy co-grinding of the drug with a pharmaceutical carrier, characterized by the use of a vibrational mill equipped with means that regulate the vibration frequency. The process, performed by modifying the frequency of vibration and keeping its amplitude constant, produces drug/carrier composites with a constant particle size in which the degree of drug activation increases in proportion to the frequency applied. The invention also includes a vibrational mill suitably modified to perform the process described.

Drug activation process and vibrational mill therefor

Process for the preparation of pharmaceutical compositions comprising one or more polymers and one or more drugs by the extrusion and spheronization technique, wherein polymers belong to the group of the cross-linked amphiphilic polymers.

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Trieste, Italy

Massimo Bresciani